Month: October 2022

HPLC of Formula: 20154-03-4In 2016 ,《Inhibitors of HIV-1 attachment: The discovery and structure-activity relationships of tetrahydroisoquinolines as replacements for the piperazine benzamide in the 3-glyoxylyl 6-azaindole pharmacophore》 was published in Bioorganic & Medicinal Chemistry Letters. The article was written by Swidorski, Jacob J.; Liu, Zheng; Yin, Zhiwei; Wang, Tao; Carini, David J.; Rahematpura, Sandhya; Zheng, Ming; Johnson, Kim; Zhang, Sharon; Lin, Pin-Fang; Parker, Dawn D.; Li, Wenying; Meanwell, Nicholas A.; Hamann, Lawrence G.; Regueiro-Ren, Alicia. The article contains the following contents:

6,6-Fused ring systems including tetrahydroisoquinolines and tetrahydropyrido[3,4-d]pyrimidines have been explored as possible replacements for the piperazine benzamide portion of the HIV-1 attachment inhibitor BMS-663068. In initial studies, the tetrahydroisoquinoline compounds demonstrate sub-nanomolar activity in a HIV-1 pseudotype viral infection assay used as the initial screen for inhibitory activity. Anal. of SARs and approaches to optimization for an improved drug-like profile are examined herein. The results came from multiple reactions, including the reaction of 3-(Trifluoromethyl)-1H-pyrazole(cas: 20154-03-4HPLC of Formula: 20154-03-4)

3-(Trifluoromethyl)-1H-pyrazole(cas: 20154-03-4) belongs to pyrazoles. Pyrazole derivatives have been reported to exhibit a wide range of applications in medicinal chemistry and pharmacology. A large number of drugs incorporating pyrazole structure have been utilized as partial agonists for nicotinic acid receptors, antidepressants, antimicrobial agents, antiviral agents, and antifungal agents solely or along with the combination of other structural motifs.HPLC of Formula: 20154-03-4

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

Recommanded Product: 844501-71-9In 2012 ,《Thienopyridine ureas as dual inhibitors of the VEGF and Aurora kinase families》 was published in Bioorganic & Medicinal Chemistry Letters. The article was written by Curtin, Michael L.; Frey, Robin R.; Heyman, H. Robin; Soni, Niru B.; Marcotte, Patrick A.; Pease, Lori J.; Glaser, Keith B.; Magoc, Terrance J.; Tapang, Paul; Albert, Daniel H.; Osterling, Donald J.; Olson, Amanda M.; Bouska, Jennifer J.; Guan, Zhiwen; Preusser, Lee C.; Polakowski, James S.; Stewart, Kent D.; Tse, Chris; Davidsen, Steven K.; Michaelides, Michael R.. The article contains the following contents:

In an effort to identify multi-targeted kinase inhibitors with a novel spectrum of kinase activity, a screen of Abbott proprietary KDR inhibitors against a broad panel of kinases was conducted and revealed a series of thienopyridine ureas with promising activity against the Aurora kinases. Modification of the di-Ph urea and C7 moiety of these compounds provided potent inhibitors with good pharmacokinetic profiles that were efficacious in mouse tumor models after oral dosing. Compound 2 (ABT-348) of this series is currently undergoing Phase I clin. trials in solid and hematol. cancer populations.3-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole(cas: 844501-71-9Recommanded Product: 844501-71-9) was used in this study.

3-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole(cas: 844501-71-9) belongs to pyrazoles. Pyrazoles are commonly used scaffold molecules in drug discovery projects. The use of pyrazole derivatives is based on their analgesic, anti-inflammatory, antipyretic, antiarrhythmic, sedative, muscle relaxant, neuroleptic, anticonvulsant, monoamine oxidase inhibitory, antidiabetic and antibacterial activities. Recommanded Product: 844501-71-9

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

Electric Literature of C12H13N3O2On May 15, 2015 ,《Synthetic studies of five-membered heteroaromatic derivatives as potassium-competitive acid blockers (P-CABs)》 appeared in Bioorganic & Medicinal Chemistry Letters. The author of the article were Arikawa, Yasuyoshi; Hasuoka, Atsushi; Nishida, Haruyuki; Hirase, Keizo; Inatomi, Nobuhiro; Takagi, Terufumi; Tarui, Naoki; Kawamoto, Makiko; Imanishi, Akio; Itoh, Fumio; Kajino, Masahiro. The article conveys some information:

On the basis of a series of novel and potent potassium-competitive acid blockers represented by 1-sulfonylpyrrole derivative I, we prepared several five-membered heterocyclic analogs II [Ht = S, N, O containing heterocycle] and evaluated their H+,K+-ATPase activities in vitro. We also assessed the role of the methylaminomethyl side chain by comparison with methylamino and ethylamino derivatives We observed that the five-membered core ring and its orientation affect inhibitory activity and that the methylaminomethyl moiety is the best side chain. On the basis of potency and ligand-lipophilicity efficiency, compound I remains the most drug-like of the compounds studied to date. This study revealed the factors necessary for potent H+,K+-ATPase inhibition, such as differences in electron d., the properties of the lone pair at each apical position of the heteroaromatic ring, and the geometry of the substituents. After reading the article, we found that the author used Ethyl 5-amino-1-phenyl-1H-pyrazole-3-carboxylate(cas: 866837-96-9Electric Literature of C12H13N3O2)

Ethyl 5-amino-1-phenyl-1H-pyrazole-3-carboxylate(cas: 866837-96-9) belongs to anime. Reaction with nitrous acid (HNO2), which functions as an acylating agent that is a source of the nitrosyl group (―NO), converts aliphatic primary amines to nitrogen and mixtures of alkenes and alcohols corresponding to the alkyl group in a complex process. This reaction has been used for analytical determination of primary amino groups in a procedure known as the Van Slyke method.Electric Literature of C12H13N3O2

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

In 2014,Ojeda-Gomez, Claudia; Pessoa-Mahana, Hernan; Iturriaga-Vasquez, Patricio; Pessoa-Mahana, Carlos David; Recabarren-Gajardo, Gonzalo; Mendez-Rojas, Claudio published 《Synthesis and Biological Screening of Novel Indolalkyl Arenes Targeting the Serotonin Transporter》.Archiv der Pharmazie (Weinheim, Germany) published the findings.Recommanded Product: 3-(Trifluoromethyl)-1H-pyrazole The information in the text is summarized as follows:

A series of functionalized indolylalkylarenes were synthesized and their affinities for the serotonin transporter were investigated in vitro. Compounds I (R = H, F; R’ = 4-CF3Ph, 2-FBn, PhCH2CH2) were obtained by nucleophilic substitution of 3-(1H-indol-3-yl)propyl-4-methylbenzenesulfonates with a series of azaheterocycles. Compounds II (R = H, F; R’ = H, Cl, NO2) were prepared in a two-step sequence by reaction of 3-(1H-indol-3-yl)-2-methylpropanal with substituted 1,2-phenylenediamines. Compounds I (R = F; R’ = 4-CF3Ph, 2-FBn, PhCH2CH2) showed good binding affinities (Ki = 33.0, 48.0, and 17 nM, resp.). The other synthesized compounds showed moderate or no affinity in the binding studies. The experimental part of the paper was very detailed, including the reaction process of 3-(Trifluoromethyl)-1H-pyrazole(cas: 20154-03-4Recommanded Product: 3-(Trifluoromethyl)-1H-pyrazole)

3-(Trifluoromethyl)-1H-pyrazole(cas: 20154-03-4) belongs to pyrazoles. The application of pyrazole derivatives in the development of anticancer agents has been thoroughly investigated and verified. Moreover, the medicinal features of a number of natural products incorporating pyrazole moiety such as pyrazofurin, pyrazofurin B, pyrazole-3(5)-carboxylic acid and 4-methylpyrazole-3(5)-carboxylic acid have been reported.Recommanded Product: 3-(Trifluoromethyl)-1H-pyrazole

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

In 2015,Parsy, Christophe C.; Alexandre, Francois-Rene; Bidau, Valerie; Bonnaterre, Florence; Brandt, Guillaume; Caillet, Catherine; Cappelle, Sylvie; Chaves, Dominique; Convard, Thierry; Derock, Michel; Gloux, Damien; Griffon, Yann; Lallos, Lisa B.; Leroy, Frederic; Liuzzi, Michel; Loi, Anna-Giulia; Moulat, Laure; Chiara, Musiu; Roques, Virginie; Rosinovsky, Elodie; Savin, Simon; Seifer, Maria; Standring, David; Surleraux, Dominique published 《Discovery and structural diversity of the hepatitis C virus NS3/4A serine protease inhibitor series leading to clinical candidate IDX320》.Bioorganic & Medicinal Chemistry Letters published the findings.Electric Literature of C4H3F3N2 The information in the text is summarized as follows:

Exploration of the P2 region by mimicking the proline motif found in BILN2061 resulted in the discovery of two series of potent HCV NS3/4A protease inhibitors. X-ray crystal structure of the ligand in contact with the NS3/4A protein and modulation of the quinoline heterocyclic region by structure based design and modeling allowed for the optimization of enzyme potency and cellular activity. This research led to the selection of clin. candidate IDX320 having good genotype coverage and pharmacokinetic properties in various species. After reading the article, we found that the author used 3-(Trifluoromethyl)-1H-pyrazole(cas: 20154-03-4Electric Literature of C4H3F3N2)

3-(Trifluoromethyl)-1H-pyrazole(cas: 20154-03-4) belongs to pyrazoles. The application of pyrazole derivatives in the development of anticancer agents has been thoroughly investigated and verified. Moreover, the medicinal features of a number of natural products incorporating pyrazole moiety such as pyrazofurin, pyrazofurin B, pyrazole-3(5)-carboxylic acid and 4-methylpyrazole-3(5)-carboxylic acid have been reported.Electric Literature of C4H3F3N2

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

Product Details of 930-36-9On May 31, 2022, Zhakupbekova, Aray; Baimatova, Nassiba; Psillakis, Elefteria; Kenessov, Bulat published an article in Environmental Science and Pollution Research. The article was 《Quantification of trace transformation products of rocket fuel unsymmetrical dimethylhydrazine in sand using vacuum-assisted headspace solid-phase microextraction》. The article mentions the following:

Quantification of unsym. dimethylhydrazine transformation products in solid samples is an important stage in monitoring of environmental pollution caused by heavy rockets launches. The new method for simultaneous quantification of unsym. dimethylhydrazine transformation products in sand samples using vacuum-assisted headspace solid-phase microextraction without addition of water followed by gas chromatog.-mass spectrometry is proposed. Decreasing air evacuation time from 120 to 20 s at 23°C resulted in increased responses of analytes by 25-46% and allowed obtaining similar responses as after evacuation at -30°C. The best combination of responses of analytes and their relative standard deviations (RSDs) was achieved after air evacuation of a sample (m = 1.00 g) for 20 s at 23°C, incubation for 30 min at 40°C, and 30-min extraction at 40°C by Carboxen/polydimethylsiloxane (Car/PDMS) fiber. The method was validated in terms of linearity (R2=0.9912-0.9938), limits of detection (0.035 to 3.6 ng g-1), limits of quantification (0.12-12 ng g-1), recovery (84-97% with RSDs 1-11%), repeatability (RSDs 3-9%), and reproducibility (RSDs 7-11%). It has a number of major advantages over existing methods based on headspace solid-phase microextraction-lower detection limits, better accuracy and precision at similar or lower cost of sample preparation The developed method was successfully applied for studying losses of analytes from open vials with model sand spiked with unsym. dimethylhydrazine transformation products. It can be recommended for anal. of trace concentrations of unsym. dimethylhydrazine transformation products when studying their transformation, migration and distribution in contaminated sand. After reading the article, we found that the author used 1-Methylpyrazole(cas: 930-36-9Product Details of 930-36-9)

1-Methylpyrazole(cas: 930-36-9) belongs to pyrazoles. Pyrazoles and their related multiring analogs are common elements of a wide variety of bioactive compounds. These ring structures are rare in nature. A consequence of this is that they have previously been thought to be poor moieties to include in potential new drugs. Product Details of 930-36-9

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

In 1998,Organic Reactions (Hoboken, NJ, United States) included an article by Rickborn, Bruce. Product Details of 5952-93-2. The article was titled 《The retro-Diels-Alder reaction. Part II. Dienophiles with one or more heteroatom》. The information in the text is summarized as follows:

A review of the article The retro-Diels-Alder reaction. Part II. Dienophiles with one or more heteroatom. In the experiment, the researchers used many compounds, for example, Methyl 1-methyl-1H-pyrazole-4-carboxylate(cas: 5952-93-2Product Details of 5952-93-2)

Methyl 1-methyl-1H-pyrazole-4-carboxylate(cas: 5952-93-2) belongs to pyrazoles. Pyrazoles and their related multiring analogs are common elements of a wide variety of bioactive compounds. These ring structures are rare in nature. A consequence of this is that they have previously been thought to be poor moieties to include in potential new drugs. Product Details of 5952-93-2

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

In 2014,Angewandte Chemie, International Edition included an article by O’Brien, Alexander G.; Maruyama, Akinobu; Inokuma, Yasuhide; Fujita, Makoto; Baran, Phil S.; Blackmond, Donna G.. Category: pyrazoles-derivatives. The article was titled 《Radical C-H functionalization of heteroarenes under electrochemical control》. The information in the text is summarized as follows:

Electrochem. reactions are shown to be effective for the C-H functionalization of a number of heterocyclic substrates that are recalcitrant to conventional peroxide radical initiation conditions. Monitoring reaction progress under electrochem. conditions provides mechanistic insight into the C-H functionalization of a series of heterocycles of interest in medicinal chem. In addition to this study using Methyl 1-methyl-1H-pyrazole-4-carboxylate, there are many other studies that have used Methyl 1-methyl-1H-pyrazole-4-carboxylate(cas: 5952-93-2Category: pyrazoles-derivatives) was used in this study.

Methyl 1-methyl-1H-pyrazole-4-carboxylate(cas: 5952-93-2) belongs to pyrazoles. Pyrazoles and their related multiring analogs are common elements of a wide variety of bioactive compounds. These ring structures are rare in nature. A consequence of this is that they have previously been thought to be poor moieties to include in potential new drugs. Category: pyrazoles-derivatives

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

Ivachtchenko, Alexandre V.; Kravchenko, Dmitry V.; Zheludeva, Valentina I.; Pershin, Dmitry G. published their research in Journal of Heterocyclic Chemistry on December 31 ,2004. The article was titled 《Synthesis of pinacol esters of 1-alkyl-1H-pyrazol-5-yl- and 1-alkyl-1H-pyrazol-4-ylboronic acids》.Quality Control of N,N-Dimethyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole-1-propanamine The article contains the following contents:

1-Substituted pyrazolylboronic acids and their pinacol esters were prepared by lithiation-borylation reaction sequence starting from bromopyrazoles. Alkylation of 4-bromo-1H-pyrazole gave 1-alkyl-4-bromo-1H-pyrazoles, which were lithiated at -80° and borylated with B(OMe)3 to give 1-R-1H-pyrazole-4-boronic acids [4a-g, R = Me, Et, Pr, (CH2)2CHMe2, (CH2)2OMe, (CH2)3NMe2, (CH2)2CH(OEt)2]. Lithiation of 4-bromo-1-(2-dimethylaminoethyl)-1H-pyrazole (2h) gave 5-lithio-derivative, which on borylation afforded 1-R1-4-Br-1H-pyrazole-5-boronic acid (8). Boronic acids 4a-g are unstable and were deborylated slowly due to hydrolysis by traces of water; the stability of boryl derivatives can be greatly enhanced by converting to corresponding pinacol boronates (10a-g). Direct lithiation of 1-R2-1H-pyrazoles by BuLi at -20° afforded 5-lithio-derivatives, which were converted to corresponding 1-R2-1H-pyrazole-5-boronic acids [17a-e; R2 = Me, iBu, Pr, (CH2)2CHMe2, (CH2)2CH(OEt)2] and their pinacol boronates (18a-e, same R2). The key step in the described methodol. is the regioselective lithiation of the pyrazole ring. The synthesized pinacolates are stable under prolonged storage and can be used as convenient reagents in organic synthesis. In the experiment, the researchers used many compounds, for example, N,N-Dimethyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole-1-propanamine(cas: 847818-72-8Quality Control of N,N-Dimethyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole-1-propanamine)

N,N-Dimethyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole-1-propanamine(cas: 847818-72-8) belongs to pyrazoles. Pyrazoles are commonly used scaffold molecules in drug discovery projects. The use of pyrazole derivatives is based on their analgesic, monoamine oxidase inhibitory, anti-inflammatory, antipyretic, neuroleptic, anticonvulsant, antiarrhythmic, sedative, muscle relaxant, antidiabetic and antibacterial activities. Quality Control of N,N-Dimethyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole-1-propanamine

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

In 2015,Lu, Zehai; Li, Qingwei; Tang, Minghua; Jiang, Panpan; Zheng, Hao; Yang, Xianjin published 《CFBSA: a novel and practical chlorinating reagent》.Chemical Communications (Cambridge, United Kingdom) published the findings.SDS of cas: 847818-74-0 The information in the text is summarized as follows:

A structurally simple and highly reactive chlorinating reagent, N-chloro-N-fluorobenzenesulfonylamine (CFBSA), was conveniently prepared from easily available inexpensive Chloramine-B in high yield. A wide range of substrates were chlorinated with CFBSA to obtained products in good to high yields and appropriate selectivity. The results came from multiple reactions, including the reaction of 1-Methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole(cas: 847818-74-0SDS of cas: 847818-74-0)

1-Methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole(cas: 847818-74-0) belongs to pyrazoles. Pyrazoles are commonly used scaffold molecules in drug discovery projects. The use of pyrazole derivatives is based on their analgesic, anti-inflammatory, antipyretic, antiarrhythmic, sedative, muscle relaxant, neuroleptic, anticonvulsant, monoamine oxidase inhibitory, antidiabetic and antibacterial activities. SDS of cas: 847818-74-0

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics